Global Patent Index - EP 0106565 A1

EP 0106565 A1 19840425 - Leukotriene antagonists, their production, and compositions containing them.

Title (en)

Leukotriene antagonists, their production, and compositions containing them.

Title (de)

Leukotrienantagonisten, deren Herstellung und diese enthaltende Zusammensetzungen.

Title (fr)

Antagonistes du leucotriène, leur préparation et compositions les contenant.

Publication

EP 0106565 A1 19840425 (EN)

Application

EP 83305587 A 19830921

Priority

US 43194482 A 19820930

Abstract (en)

Compounds of the formulae: <CHEM> and their pharmaceutically acceptable (including acid-addition) salts, which are novel, are antagonists of leukotrienes of C4, D4 and E4, the slow reacting substance of anaphylaxis. They can be made into pharmaceutical compositions by incorporating them in a pharmaceutical carrier. In the formulae, each R is H, OH, SH C1 6 alkyl C2 6 alkenyl, CF3, C1 6 alkoxy, C1 6 alkylthio, benzyl, phenethyl, halogen, amino, N(R4)2, COOR4 or CH2OR4 where R4 is H or C1 6 alkyl, formyl, CN, CF3S or NO2; each R min is R4; OR4; COOR4; N(R4)2; SR4; CH2OR4 or CHO; or together R min and R min are O, CH2 or <CHEM> Y min is sulfur, sulfoxide, sulfone, @ = NR11, = NR12, = N - CO - R13, - N - CN, CH2 or C = 0 where R11 is H, C1-4 alkyl, C1 4 alkanoyl, phenylsulfonyl or p-toluenesulfonyl, R12 is H or C1-4 alkyl and R13 is C1-4 alkyl or C1-4 alkoxy; Y is of the type defined for Y min or oxygen; each R1 is hydrogen C1-3 alkyl; each m is 0 or an integer from 1 to 6; <CHEM> where each R6 is H or C1-4 alkyl; each R7 is H, OH or C1-4 alkyl; and each R8 is H or C1-4 alkyl and is absent when the two indicated carbons are triply bonded; R5 is COOR4; CH2OH, CHO: tetrazole; NHSO2R14; CONHSO2R14; hydroxymethylketone; CN; CON(R7)2; a monocyclic or bicyclic heterocyclic ring containing an acidic hydroxyl group; or COOR15 where R15 is: <CHEM> where each s is independently 0-3, R6 is as defined above and R16 is (A) a monocyclic or bicyclic heterocyclic radical containing from 3 to 12 nuclear carbon atoms and 1 or 2 N heteroatoms or one N and one S heteratom, each ring in the heterocyclic radical being formed of 5 or 6 atoms, or (B) W-R17 where W is O, S or NH and R17 contains up to 21 carbon atoms and is (1) a hydrocarbon radical or (2) an acyl radical or an organic acyclic or monocyclic carboxylic acid containing not more than 1 heteroatom in the ring; each of r and q is 0-20 but r + q does not exceed 20; and p is 0 or 1; R3 is C1-6 alkyl or C3-6 alkenyl; R9 is C1-6 alkyl, C1 6 alkoxy or (CH2)rR5, where r and R5 are as defined above; and R10 is H, C1-6 alkyl; R4CO- or R4OCH2, where R4 is as defined above and R14 is OH, C1-6 alkoxy, C1-6 acyl, phenyl, phenyl having C1-3 alkyl or C1-3 alkoxy substitution, halogen, halogenated alkyl, carboxy, cyano or formyl.

IPC 1-7

C07C 149/40; C07C 147/14; C07C 147/107; C07C 59/90; C07C 59/64; C07C 51/347; A61K 31/19

IPC 8 full level

C07C 59/40 (2006.01); A61K 31/12 (2006.01); A61K 31/135 (2006.01); A61K 31/165 (2006.01); A61K 31/18 (2006.01); A61K 31/19 (2006.01); A61K 31/21 (2006.01); A61K 31/215 (2006.01); A61P 9/00 (2006.01); A61P 11/00 (2006.01); A61P 29/00 (2006.01); A61P 37/08 (2006.01); A61P 43/00 (2006.01); C07C 45/46 (2006.01); C07C 45/71 (2006.01); C07C 49/84 (2006.01); C07C 51/00 (2006.01); C07C 51/347 (2006.01); C07C 59/64 (2006.01); C07C 59/90 (2006.01); C07C 67/00 (2006.01); C07C 239/00 (2006.01); C07C 261/04 (2006.01); C07C 313/00 (2006.01); C07C 317/00 (2006.01); C07C 317/24 (2006.01); C07C 317/28 (2006.01); C07C 317/36 (2006.01); C07C 317/44 (2006.01); C07C 317/46 (2006.01); C07C 317/48 (2006.01); C07C 323/12 (2006.01); C07C 323/19 (2006.01); C07C 323/22 (2006.01); C07C 323/25 (2006.01); C07C 323/52 (2006.01); C07C 323/62 (2006.01); C07C 325/00 (2006.01); C07C 381/10 (2006.01)

CPC (source: EP)

A61P 9/00 (2017.12); A61P 11/00 (2017.12); A61P 29/00 (2017.12); A61P 37/08 (2017.12); A61P 43/00 (2017.12); C07C 45/46 (2013.01); C07C 45/71 (2013.01); C07C 49/84 (2013.01); C07C 59/90 (2013.01); C07C 255/00 (2013.01); C07C 317/00 (2013.01); C07C 323/00 (2013.01)

Citation (search report)

Designated contracting state (EPC)

AT BE CH DE FR GB IT LI LU NL SE

DOCDB simple family (publication)

EP 0106565 A1 19840425; EP 0106565 B1 19860910; AT E22072 T1 19860915; CA 1273349 A 19900828; DE 3366107 D1 19861016; DK 446383 A 19840331; DK 446383 D0 19830929; ES 526065 A0 19850401; ES 8503636 A1 19850401; JP S5993043 A 19840529

DOCDB simple family (application)

EP 83305587 A 19830921; AT 83305587 T 19830921; CA 437653 A 19830927; DE 3366107 T 19830921; DK 446383 A 19830929; ES 526065 A 19830929; JP 18099883 A 19830930